Synthesis, structure–activity relationships and preliminary antitumor evaluation of benzothiazole-2-thiol derivatives as novel apoptosis inducers

SKLB316, a novel small-molecule inhibitor of cell-cycle progression, induces G2/M phase arrest and apoptosis in vitro and inhibits tumor growth in vivo

“…SKLB316 has been developed via computer-aided drug design, structural modification of benzothiazole-2-thiol derivatives [18,32], and de novo synthesis. In the present study, we investigated the activities of SKLB316 to inhibit colorectal and pancreatic cancer in vitro and in vivo and the possible mechanism.…”

A comprehensive review in current developments of benzothiazole-based molecules in medicinal chemistry

“…Compounds (90,91) exhibited good antitumor activities against the different types of human cancer cell lines in vitro, with IC 50 values ranging from 1.1 to 8.8 mM. The SAR study reveals that chloromethyl could improve significantly the antitumor activity of this series of BTA derivatives [130]. N-Fluoroalkyl-N'-benzothiazolyl ureas 92(aec) were synthesized by Luzina and Popov, studied their in vitro antiproliferative activities against the human diseaseoriented tumor cell lines MCF7 (breast), NCIeH460 (lung), and SF-268 (CNS).…”

A novel inhibitor of Rho GDP-dissociation inhibitor α improves the therapeutic efficacy of paclitaxel in Lewis lung carcinoma

“…SKLB-163) was developed via computer-aided drug design and de novo synthesis in our laboratory. Our data exhibited that SKLB-163 had good anticancer activities in vitro and in vivo (9,10). The molecular mechanism is involved as follows: SKLB-163 inhibited the upstream RhoGDIα protein and activated that c-Jun N-terminal kinase 1 signaling pathway that could contribute to the activation of caspase-3, decreased level of phosphorylated mitogen-activated protein kinase and AKT.…”

“…The route adapted for the synthesis of the SKLB-163 compound was performed as previously described (10). SKLB-163 was dissolved in dimethyl sulfoxide (DMSO) as a stock solution and was stored at 4˚C.…”